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http://gi.dxy.cn/article/542453
Main Text
Metoclopramide (also known as Gastrocom, Reglan) is a dopamine 2 (D2) receptor antagonist. It also acts as an agonist of 5-hydroxytryptamine 4 (5-HT4) receptors and mildly inhibits 5-hydroxytryptamine 3 (5-HT3) receptors. It has central antiemetic effects and promotes gastric and esophageal motility, and is widely used in clinical departments.
However, have you accurately avoided these 8 “minefields” in the use of metoclopramide?
- Can it be used in patients with breast tumors?
Package Insert Contraindications: Not to be used in breast cancer patients vomiting due to chemotherapy and radiotherapy.
Analysis: Metoclopramide can increase the relative content and activity of estrogen, leading to long-term overstimulation of breast tissue by estradiol, causing breast lesions. Both ESMO and ASCO antiemetic guidelines do not recommend the use of Gastrocom for nausea and vomiting after chemotherapy in breast cancer patients.
Controversy: The “Chinese Anti-Cancer Association Breast Cancer Diagnosis and Treatment Guidelines and Standards (2017 edition)” recommend its use [1], while the American guidelines and “Martindale: The Complete Drug Reference” do not list breast cancer as a contraindication.
Suggestion: Avoid using in breast cancer patients; use 5-hydroxytryptamine inhibitors instead. If other antiemetics are ineffective or there is explosive vomiting, it can be used temporarily.
- Can it be used for pregnancy-related vomiting?
Package Insert for Pregnant Women: Potential teratogenic effect; not suitable for use during pregnancy.
Controversy: The “Expert Consensus on Diagnosis and Clinical Management of Hyperemesis Gravidarum (2015)” mentions that metoclopramide can be used throughout pregnancy with no evidence of adverse effects on embryos, fetuses, or newborns [2]. Some literature confirms that metoclopramide is safe for vomiting in early pregnancy [3].
Suggestion: Metoclopramide can be chosen for vomiting during pregnancy, but adverse reactions such as drowsiness, dry mouth, and ketonuria should be monitored.
- Can it be used in patients with gastrointestinal bleeding?
Package Insert Contraindications: Gastrointestinal bleeding, mechanical intestinal obstruction or perforation, as increased gastrointestinal motility caused by the drug may worsen the condition.
Special Circumstances: Helps improve visibility during endoscopic hemostasis [4] (not recommended in domestic guidelines, erythromycin is recommended [5]).
- Can it be used for vomiting caused by motion sickness?
Package Insert Precautions: Ineffective for vomiting caused by motion sickness.
Analysis: Motion sickness is mainly a syndrome of vestibular and autonomic nervous system reactions (imbalance). Main treatments include anticholinergics (scopolamine), antihistamines (diphenhydramine), calcium channel blockers (flunarizine), etc., and metoclopramide is mentioned as having some effect [6].
Suggestion: Not the first choice for vomiting caused by motion sickness.
- Can it be combined with scopolamine (or atropine)?
Package Insert Drug Interactions: Antagonistic effects when combined with anticholinergic drugs and anesthetic analgesics.
Special Circumstances: For patients with biliary colic accompanied by vomiting, the two drugs have complementary effects.
Reason: Metoclopramide’s effect on biliary smooth muscle is different from its effect on the gastrointestinal tract; it not only does not excite but also relaxes the biliary sphincter, regulating bile duct movement and bile secretion; in addition, it has sedative and abdominal pain relieving effects.
- Can it be combined with digoxin (or vitamin B2, cimetidine)?
Digoxin Package Insert: Metoclopramide reduces the bioavailability of digoxin by about 25% due to promoting intestinal motility.
Metoclopramide Package Insert: When combined with slow-release digoxin formulations, gastrointestinal absorption of digoxin is reduced; spacing administration by 2 hours can reduce this effect; also increases biliary excretion of digoxin, altering its blood concentration.
Analysis: Digoxin is absorbed at the upper small intestine. Metoclopramide accelerates intestinal peristalsis, causing digoxin to pass through the small intestine before being fully dissolved and absorbed.
Suggestion: When using digoxin, metoclopramide should not be used simultaneously; trimebutine (which regulates abnormal gastric motility) can be used instead, or administer with an interval of over 2 hours.
- Can it be combined with chlorpromazine?
Metoclopramide Package Insert: When combined with drugs that cause extrapyramidal reactions, such as phenothiazines (chlorpromazine, prochlorperazine), the incidence and severity of extrapyramidal reactions may increase.
Suggestion: Space use by over 2 hours; increase awareness of extrapyramidal adverse reactions to avoid misdiagnosis; in case of extrapyramidal reactions, treat with benzhexol (3–5 days to prevent recurrence), diphenhydramine, or scopolamine (for emergency) [7].
- Can it be administered by intravenous infusion?
Package Insert Usage: Intramuscular or intravenous injection.
The “National Formulary (2010/2013 Pediatric Edition)” and “Clinical Medication Instructions (2010 Edition)” regarding metoclopramide usage and dosage: intramuscular injection, intravenous drip; use when necessary, for patients who cannot take orally or for treatment of acute vomiting. Therefore, metoclopramide can be administered intravenously (10–20 mg per dose).
Originally published by: Gastrointestinal Time
Editors: Li Qing, Ziyan
Featured image source: shutterstock
For submissions and cooperation: sunzy@dxy.cn
References:
[1] Chinese Anti-Cancer Association Breast Cancer Diagnosis and Treatment Guidelines and Standards (2017 Edition)
[2] Expert Consensus on Diagnosis and Clinical Management of Hyperemesis Gravidarum (2015)
[3] Matok I1, Gorodischer R, Koren G, The safety of metoclopramide use in the first trimester of pregnancy. N Engl J Med. 2009 Jun 11;360(24):2528-35.
[4] 2013+ WSES Statement: Diagnosis and Treatment of Peptic Ulcer Perforation or Bleeding.
[5] Guidelines for Diagnosis and Treatment of Acute Non-Variceal Upper Gastrointestinal Bleeding (2015, Nanchang)
[6] Liu Yuanyuan, Fu Wei, et al. Progress in Research on Drugs for Prevention and Treatment of Motion Sickness, International Journal of Pharmaceutical Research, 2014,5.
[7] Ren Hong, Analysis of 13 Cases of Misdiagnosed Extrapyramidal Reactions Caused by Metoclopramide, Chinese Journal of Practical Neurological Diseases, 2011,14(9):92.
Editor: Huang Jianqin